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TIC10 (TRAIL-inducing compound 10) is a potent and stable small molecule that is orally active. It induces TRAIL transcriptionally independent of p53 and crosses the blood-brain barrier. [1]

Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) is an apoptosis inducer in a variety of human cancer cell lines. It also acts as a tumor suppressor during immune surveillance but the function is lost in cancer progression. [1]

TIC10 caused a prominent and long-lasting production of TRAIL on cell surface of tumor cell.

TIC10 also led to TRAIL-mediated apoptosis in HCT116 p53-/- cells. In addition, TIC10 inactivated Akt and ERK cooperatively lead to the nuclear translocation of Foxo3a and ensuing TRAIL up-regulation. [1]

In mouse caner xenograft, TIC10 showed TRAIL-dependent antitumor effect. It caused tumor-specific cell death by RAIL-mediated direct and bystander effects. TIC10 is also an effective antitumor agent for orthotopic human glioblastoma multiforme tumors. [1]

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